Assay Detail
Binding
CHEMBL2060155
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Inhibition of BuChE in Wistar rat plasma using acetylthiocholine iodide as substrate after 0.5 hrs by Ellman's method
32
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of phenserine analogues and evaluation of their cholinesterase inhibitory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.76 | 7.23 |
| Inhibition | 16 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL94 | PHYSOSTIGMINE | 3.0 | 2 | 7.23 |
| CHEMBL2058983 | — | — | 2 | 4.52 |
| CHEMBL54727 | — | — | 2 | 4.52 |
| CHEMBL2059199 | — | — | 2 | 4.44 |
| CHEMBL2058987 | — | — | 2 | 4.38 |
| CHEMBL2058985 | — | — | 2 | 4.18 |
| CHEMBL2058980 | — | — | 2 | 4.06 |
| CHEMBL2058976 | — | — | 2 | - |
| CHEMBL2058978 | — | — | 2 | - |
| CHEMBL2058977 | — | — | 2 | - |
| CHEMBL2058979 | — | — | 2 | - |
| CHEMBL2058981 | — | — | 2 | - |
| CHEMBL2058982 | — | — | 2 | - |
| CHEMBL2058984 | — | — | 2 | - |
| CHEMBL2058986 | — | — | 2 | - |
| CHEMBL2059200 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL94 | PHYSOSTIGMINE | IC50 | = | 58.4 | nM | 7.23 |
| CHEMBL2058983 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL54727 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL2059199 | — | IC50 | = | 36200.0 | nM | 4.44 |
| CHEMBL2058987 | — | IC50 | = | 41900.0 | nM | 4.38 |
| CHEMBL2058985 | — | IC50 | = | 65300.0 | nM | 4.18 |
| CHEMBL2058980 | — | IC50 | = | 87300.0 | nM | 4.06 |
| CHEMBL2059199 | — | Inhibition | - | % | - | |
| CHEMBL2058978 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2059200 | — | Inhibition | - | % | - | |
| CHEMBL54727 | — | Inhibition | - | % | - | |
| CHEMBL2058976 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2059200 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2058986 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2058984 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2058982 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2058981 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2058979 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2058977 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2058976 | — | Inhibition | - | % | - | |
| CHEMBL2058978 | — | Inhibition | - | % | - | |
| CHEMBL2058977 | — | Inhibition | - | % | - | |
| CHEMBL2058979 | — | Inhibition | - | % | - | |
| CHEMBL2058981 | — | Inhibition | - | % | - | |
| CHEMBL2058980 | — | Inhibition | - | % | - | |
| CHEMBL2058982 | — | Inhibition | - | % | - | |
| CHEMBL2058983 | — | Inhibition | - | % | - | |
| CHEMBL2058984 | — | Inhibition | - | % | - | |
| CHEMBL2058985 | — | Inhibition | - | % | - | |
| CHEMBL2058986 | — | Inhibition | - | % | - | |
| CHEMBL94 | PHYSOSTIGMINE | Inhibition | - | % | - | |
| CHEMBL2058987 | — | Inhibition | - | % | - |